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    • 2. 发明申请
    • METHOD FOR PREPARING [18F]FALLYPRIDE WITH LOW BASE CONCENTRATION
    • 用于制备具有低碱浓度的[18F] FALLYPRIDE的方法
    • WO2011030981A1
    • 2011-03-17
    • PCT/KR2010/001351
    • 2010-03-04
    • SNU R&DB FOUNDATIONKIM, Sang EunLEE, Byung ChulMOON, Byung SeokKIM, Yu Kyeong
    • KIM, Sang EunLEE, Byung ChulMOON, Byung SeokKIM, Yu Kyeong
    • C07D207/14A61K31/40A61P21/00
    • C07D207/09
    • A method for preparing [ 18 F]fallypride is disclosed, which comprises a first step for trapping a fluorine-18 to a polymer ion exchange cartridge; a second step for extraction of fluorine-18 by inputting low base concentrations: 5.0~25μL of 40% TBAHCO 3 or K2.2.2./K 2 CO 3 (5~25mg/0.5~3.0 mg) as a phase-transfer catalyst in a mixture of alcohol/water(1.0/0.2(v/v)) or alcohol as a solvent into the polymer ion exchange cartridge trapped by the fluorine-18; a third step for preparing a [ 18 F]fallypride product by removing the solvent from the trapped fluorine-18, by inputting tosylate precursor in CH 3 CN as a solvent into a reactor and by reacting the same for 5~35 minutes at 50~120°C; and a fourth step for preparing a pure [ 18 F]fallypride by purifying the prepared [ 18 F]fallypride product. The present invention makes it possible to improve the radiochemical yield of [ 18 F]fallypride, the improvement of which was a problem in the conventional automated method, by more than about 50% while reducing the preparation time by about 20 minutes. The present invention can be well applied to a clinical research by the positron emission tomography (PET).
    • 公开了一种制备[18 F]菲拉必利的方法,其包括将氟-18捕获到聚合物离子交换盒的第一步骤; 通过输入低碱浓度来提取氟-18的第二步:将5.0〜25μL40%TBAHCO 3或作为相转移催化剂的K2​​.2.2./K2CO3(5〜25mg / 0.5〜3.0mg)在醇的混合物中 /水(1.0 / 0.2(v / v))或醇作为溶剂进入被氟-18捕获的聚合物离子交换柱; 将通过在CH 3 CN中的甲苯磺酸酯前体作为溶剂输入反应器并通过在50〜120℃下反应5〜35分钟,通过从捕获的氟-18中除去溶剂来制备[18 F] fallypride产物的第三步骤 ; 以及通过纯化制备的[18 F] fallypride产物制备纯的[18 F] fallypride的第四步骤。 通过本发明,可以提高常规自动化方法中的改善成为问题的[18F] fallypride的放射化学产率超过约50%,同时将制备时间缩短约20分钟。 本发明可以很好地应用于正电子发射断层摄影(PET)的临床研究。